Oral care compositions

ABSTRACT

This application provides, among other things, novel aqueous oral care compositions useful for combining and delivering poorly compatible ingredients, for example to deliver effective levels of cationic antibacterial agents in combination with short chain polyphosphate salts that protect against erosion and staining, by addition of a stabilizing amount of an anionic surfactant and methods for making and using the same.

CROSS-REFERENCE TO RELATED APPLICATIONS

This application is a national application filed under 35 U.S.C. §111,which is a continuation application claiming priority to and thebenefit of U.S. application Ser. No. 15/667,698, filed on Aug. 3, 2017,which claims priority to and the benefit of U.S. provisional application62/373,567, filed on Aug. 11, 2016, the contents of which areincorporated by reference herein in their entireties.

BACKGROUND

This application relates, inter alia, to novel aqueous oral carecompositions useful for combining and delivering poorly compatibleingredients, for example to deliver effective levels of cationicantibacterial agents in combination with polyphosphate salts thatprotect against erosion and staining.

Biofilms form when bacteria adhere to surfaces in some form of wateryenvironment and begin to excrete a slimy, glue-like substance that canstick to all kinds of materials—metals, plastics, soil particles,medical implant materials, biological tissues. Dental plaque is abiofilm that adheres to tooth and other oral surfaces, particularly atthe gingival margin, and is implicated in the occurrence of gingivitis,periodontitis, caries and other forms of periodontal disease. Dentalplaque is cohesive and highly resistant to removal from teeth and/ororal surfaces. Bacteria associated with dental plaque convert sugar toglucans, which are insoluble polysaccharides that provide plaque withits cohesive properties. Anaerobic bacteria in plaque metabolize sugarto produce acids which dissolve tooth minerals, damaging the enamel andeventually forming dental caries. Saliva can buffer acids produced bybacteria and promote remineralization of the enamel, but extensiveplaque can block the saliva from contact with the enamel. Redepositionof minerals in the biofilm forms a hard deposit on the tooth calledcalculus (or tartar), which becomes a local irritant for the gums,causing gingivitis.

Various antibacterial agents can retard the growth of bacteria and thusreduce the formation of biofilm on oral surfaces. In many cases, theseantibacterial agents are cationic, for example quaternary ammoniumsurfactants such as cetyl pyridinium chloride (CPC), bisguanides such aschlorhexidine, metal cations such as zinc or stannous ions, andguanidines such as arginine.

Everyday activities such as smoking or other oral use of tobaccoproducts, and eating, chewing or drinking certain foods and beverages(particularly coffee, tea, cola drinks, and red wine), cause undesirablestaining of surfaces of teeth. Staining can also result from microbialactivity, including that associated with dental plaque. The chromogensor color causing substances in these materials become part of thepellicle layer and can permeate the enamel layer. Even with regularbrushing and flossing, years of chromogen accumulation can impartnoticeable tooth discoloration.

A tooth is comprised of an inner dentin layer and an outer hard enamellayer that is the protective layer of the tooth. The enamel layer of atooth is naturally opaque, and white or a slightly off-white color. Theenamel layer is composed of hydroxyapatite mineral crystals that createa somewhat porous surface. These hydroxyapatite crystals formmicroscopic hexagonal rods or prisms that make up the enamel surface. Asa result, the surface of the enamel presents microscopic spaces or poresbetween the prisms. Without limiting the mechanism, function, or utilityof the present disclosure, it is believed that this porous nature of theenamel is where discoloring substances permeate the enamel and discolorthe teeth.

Since the compounds that stain the teeth are typically anionicmaterials, cationic antibacterial agents can cause or enhance stainingby facilitating the deposit of chromogens or by forming salts withminerals.

One approach to reducing staining and erosion as well as reducingbiofilm formation is the use of a dentifrice, such as a mouthwash,containing mineral agents useful in stain removal. Polyphosphate salts,for example, exhibit significant stain fighting ability, and when usedin oral care products, they deposit onto and protect the tooth surface,as well as complexing with free calcium, thereby starving bacteria andreducing calculus deposition. However, when phosphates are combined withcationic antibacterial agents, particularly in high water formulationswhere the two can readily interact in solution, the phosphates and thecationic antibacterial agents can complex to form insolubleprecipitates, thereby inactivating both components.

There is thus a need for novel oral compositions and methods thatinhibit staining and biofilm formation, and in particular that canprovide both the anti-staining and anti-calculus benefits of phosphatesand also the anti-bacterial and anti-biofilm benefits of a cationicantibacterial agent.

BRIEF SUMMARY

It is surprisingly found that addition of a stabilizing amount of ananionic surfactant, e.g. sodium lauryl sulfate, to formulationscomprising a short chain polyphosphate salt and a cationic antibacterialagent inhibits the association of these components and enhances deliveryto the teeth.

For example, quaternary ammonium antimicrobial agents such as cetylpyridinium chloride (CPC) are generally incompatible with anionicpolyphosphate salts because of the resulting precipitation of bothcomponents. However, we have found that the addition of an anionicsurfactant, such as sodium lauryl sulfate, provides needed stability andcompetition between the phosphates, the sulfate group of the surfactant,and the CPC—the result is to free CPC and make it more available forinteraction with bacteria. In some embodiments, the addition of anonionic surfactant, such as a poloxamer, e.g., poloxamer 407, furtherimproves CPC availability through additional competition pathwaysbetween water, the sulfate group of the anionic surfactant, and the CPC.Without the anionic surfactant (and optionally the nonionic surfactant),a formulation with CPC and phosphate salts may have little betterefficacy than a non-CPC containing material, or the media control.

Similarly, bisguanide antimicrobial agents such as chlorhexidine willgenerally complex with anionic polyphosphate salts no matter what stepsare taken, given their high charge density and entropically drivenprecipitation reaction. Chlorhexidine will also react with anionicsurfactants such as sodium lauryl sulfate and thus is often consideredincompatible with SLS. See, e.g. Barkvoll, et al., “Interaction betweenchlorhexidine digluconate and sodium lauryl sulfate in vivo,” J ClinPeriodontol. (1989) 16 (9):593-5.

But we have found that chlorhexidine and short chain polyphosphate saltscan be formulated in such a way to prevent precipitation (or tore-dissolve the precipitate) through the inclusion of low levels ofanionic surfactant, such as sodium lauryl sulfate (SLS). Additionalsurfactant, particularly nonionic surfactant, e.g., poloxamers, can beused in addition to the anionic surfactant and help solubilize thecomponents of the formulation.

The cationic antimicrobial agents which can be stabilized in formulationwith short chain linear polyphosphates and anionic surfactant mayalternatively be selected from, or may further comprise, for exampleantimicrobial guanidinium polymers, e.g., as disclosed in WO 2010134904A1, the contents of which are incorporated by reference herein, e.g.,polymers or co-polymers of allylguanidine compounds and salts thereof;as well as cationic amino acids and/or metal cations.

The disclosure thus provides, in one embodiment, oral care compositionscomprising:

-   -   (i) a short chain linear polyphosphate salt, for example a        phosphate salt comprising a pyrophosphate or triphosphate anion        and an alkali metal cation (e.g., potassium or sodium), for        example selected from sodium tripolyphosphate, potassium        tripolyphosphate, tetrasodium pyrophosphate, tetrapotassium        pyrophosphate, and mixtures thereof;    -   (ii) an effective amount of orally acceptable cationic active        agent, in free or orally acceptable salt form, e.g., selected        from one or more of quaternary ammonium surfactants (such as        cetyl pyridinium chloride (CPC)); bisguanides (e.g., orally        acceptable salts of chlorhexidine, such as chlorhexidine        digluconate, or of poly(hexamethylene biguanide), e.g.,        polihexanide); cationic amino acids (such as arginine, in free        or salt form); antimicrobial guanidinium polymers; metal cations        (such as zinc, calcium, or stannous ions; e.g., wherein the        cation source is a metal salt or oxide, e.g., comprises stannous        chloride, stannous fluoride, zinc citrate, zinc lactate, zinc        phosphate, zinc oxide, or combinations thereof), or combinations        thereof;    -   (iii) a stabilizing amount of an anionic surfactant, such as        sodium, potassium, ammonium, and ethanolammonium salts of linear        C₈-C₁₈ alkyl sulfates or C₈-C₁₈ alkyl ether sulfates, e.g.,        sodium laureth sulfate, sodium lauryl sulfate, ammonium lauryl        sulfate; and    -   (iv) optionally an orally acceptable nonionic surfactant, for        example selected from poloxamers, polyoxyethylenes and        combinations thereof; and    -   (v) water.

The disclosure further provides methods of inhibiting dental erosion,staining, and/or biofilm formation comprising administering to the oralcavity a composition as described.

Further areas of applicability of the present invention will becomeapparent from the detailed description provided hereinafter. It shouldbe understood that the detailed description and specific examples, whileindicating the preferred embodiment of the invention, are intended forpurposes of illustration only and are not intended to limit the scope ofthe invention.

DETAILED DESCRIPTION

The following description of the preferred embodiment(s) is merelyexemplary in nature and is in no way intended to limit the invention,its application, or uses.

As used throughout, ranges are used as shorthand for describing each andevery value that is within the range. Any value within the range can beselected as the terminus of the range. In addition, all references citedherein are hereby incorporated by referenced in their entireties. In theevent of a conflict in a definition in the present disclosure and thatof a cited reference, the present disclosure controls.

Unless otherwise specified, all percentages and amounts expressed hereinand elsewhere in the specification should be understood to refer topercentages by weight. The amounts given are based on the active weightof the material.

As is usual in the art, the compositions described herein are sometimesdescribed in terms of their ingredients, notwithstanding that theingredients may disassociate, associate or react in the formulation.Ions, for example, are commonly provided to a formulation in the form ofa salt, which may dissolve and disassociate in aqueous solution. It isunderstood that the invention encompasses both the mixture of describedingredients and the product thus obtained.

In a first embodiment, the disclosure provides oral care compositions(Composition 1) comprising:

-   -   (i) a short chain polyphosphate salt;    -   (ii) an effective amount of orally acceptable cationic active        agent, in free or orally acceptable salt form;    -   (iii) a stabilizing amount of an anionic surfactant; and    -   (iv) water.

For example, the disclosure provides embodiments of Composition 1 asfollows:

-   -   1.1 Composition 1 wherein the short chain polyphosphate salt        comprises a phosphate chain of three phosphates or less and a        monovalent cation.    -   1.2 Any foregoing composition wherein the short chain        polyphosphate salt comprises a pyrophosphate or triphosphate        anion and an alkali metal cation, e.g., selected from sodium,        potassium and combinations thereof.    -   1.3 Any foregoing composition wherein the short chain        polyphosphate salt comprises sodium tripolyphosphate,        tetrasodium pyrophosphate, tetrapotassium pyrophosphate or        combinations thereof.    -   1.4 Any foregoing composition wherein the short chain        polyphosphate salt comprises sodium tripolyphosphate.    -   1.5 Any foregoing composition wherein the short chain        polyphosphate salt is present in an amount of 0.01 wt. % to 5.0        wt. %, 0.1 wt. % to 5.0 wt. %, 0.1 wt. % to 3 wt. %, 0.5 wt. %        to 1.5 wt. %, or 1.0 wt. % based on the total weight of the        composition.    -   1.6 Any foregoing composition wherein the orally acceptable        cationic active agent is selected from one or more of quaternary        ammonium surfactants (such as cetyl pyridinium chloride (CPC),        bisguanides (such as chlorhexidine digluconate), cationic amino        acids (such as arginine), metal cations (such as zinc, calcium,        or stannous ions), guanidinium polymers, or combinations        thereof.    -   1.7 Any foregoing composition wherein the orally acceptable        cationic active agent is selected from one or more of quaternary        ammonium surfactants (such as cetyl pyridinium chloride (CPC));        bisguanides (e.g., orally acceptable salts of chlorhexidine,        e.g., chlorhexidine digluconate, or poly(hexamethylene        biguanide), e.g., polihexanide; cationic amino acids (such as        arginine, in free or salt form); antimicrobial guanidinium        polymers; metal cations (such as zinc, calcium, or stannous        ions; e.g., wherein the cation source is a metal salt or oxide,        e.g., comprises stannous chloride, stannous fluoride, zinc        citrate, zinc lactate, zinc phosphate, zinc oxide, or        combinations thereof), or combinations thereof.    -   1.8 Any foregoing composition wherein the orally acceptable        cationic active agent is selected from one or more of quaternary        ammonium surfactants (such as cetyl pyridinium chloride (CPC))        and bisguanides (e.g., orally acceptable salts of chlorhexidine,        e.g., chlorhexidine digluconate, or poly(hexamethylene        biguanide), e.g., polihexanide.    -   1.9 Any foregoing composition wherein the orally acceptable        cationic active agent comprises a pyridinium surfactant, e.g.,        cetyl pyridinium chloride (CPC).    -   1.10 Any foregoing composition wherein the orally acceptable        cationic active agent comprises chlorhexidine, in free base or        orally acceptable salt form, e.g., chlorhexidine digluconate.    -   1.11 Any foregoing composition wherein the orally acceptable        cationic active agent comprises arginine.    -   1.12 Any foregoing composition wherein the orally acceptable        cationic active agent comprises zinc ions.    -   1.13 Any foregoing composition wherein the orally acceptable        cationic active agent is provided by an orally acceptable salt        selected from zinc salts, stannous salts, pyridinium salts, and        bisguanide salts.    -   1.14 Any foregoing composition wherein the orally acceptable        cationic active agent comprises metal ions supplied by one or        more of stannous chloride, stannous fluoride, zinc citrate, zinc        lactate, zinc phosphate, and zinc oxide.    -   1.15 Any foregoing composition wherein the orally acceptable        cationic active agent is provided by an orally acceptable salt        selected from cetyl pyridinium chloride and chlorhexidine        digluconate.    -   1.16 Any foregoing composition wherein the orally acceptable        cationic active agent is provided by an orally acceptable zinc        salt, stannous salt or combination thereof.    -   1.17 Any foregoing composition wherein the effective amount of        cationic active agent, in free or salt form, is present and        comprises cetyl pyridinium chloride, in an amount of 0.05 to        0.1%, e.g., about 0.075%.    -   1.18 Any foregoing composition wherein the effective amount of        cationic active agent, in free or salt form, is present and        comprises chlorhexidine digluconate, in an amount of 0.1 to        0.2%, e.g., about 0.12%.    -   1.19 Any foregoing composition wherein the anionic surfactant        comprises an alkyl sulfate or an alkyl ether sulfate in free or        orally acceptable salt form.    -   1.20 Any foregoing composition wherein the anionic surfactant        comprises a sodium, potassium, ammonium, and ethanolammonium        salts of linear C8-C18 alkyl sulfate or C8-C18 alkyl ether        sulfate.    -   1.21 Any foregoing composition wherein the anionic surfactant        comprises sodium laurel ether sulfate (SLES), sodium lauryl        sulfate, and ammonium lauryl sulfate.    -   1.22 Any foregoing composition wherein the anionic surfactant        comprises sodium laurel sulfate.    -   1.23 Any foregoing composition wherein the anionic surfactant is        present in an amount sufficient to substantially interfere with        interaction between a cationic active agent and the short chain        polyphosphate salt, e.g. an amount sufficient to inhibit        formation of a precipitate or reduction of the efficacy of the        cationic active agent.    -   1.24 Any foregoing composition wherein the anionic surfactant is        present in an amount of 0.01 to 5.0%, 0.1 to 2.0%, 0.1 to 1.0%,        0.2 to 0.4%, or about 0.33%.    -   1.25 Any foregoing composition further comprising a nonionic        surfactant.    -   1.26 Any foregoing composition comprising a nonionic surfactant        selected from poloxamers or polyoxyethylene, poloxamer 407.    -   1.27 Any foregoing composition comprising a nonionic surfactant        which is a block copolymer of polyethylene glycol and        polypropylene glycol.    -   1.28 Any foregoing composition comprising a nonionic surfactant        in an amount of about 0.01 to 5.0%, 0.1 to 2.0%, 0.1 to 0.6%,        0.2 to 0.4%, about 0.2%, or about 0.5%.    -   1.29 Any foregoing composition comprising a nonionic surfactant        wherein the ratio of anionic surfactant to nonionic surfactant        is about 5:1 to about 1:5; about 2:1 to about 1:2; about 1.5:1        to about 1:1.5; about 1.6:1; or about 1:1.5.    -   1.30 Any foregoing composition further comprising an amino acid        or a polyamine, in free or orally acceptable salt form.    -   1.31 Any foregoing composition comprising a polyamine, in free        or orally acceptable salt form, selected from lysine or        arginine, in free or orally acceptable salt form.    -   1.32 Any foregoing composition wherein the composition comprises        0.01%-5% lysine, e.g., 0.5%-1.0% lysine, in free or orally        acceptable salt form.    -   1.33 Any foregoing composition wherein the composition comprises        0.01%-5% arginine, e.g., 0.4%-0.8% arginine, in free or orally        acceptable salt form.    -   1.34 Any foregoing composition wherein the composition comprises        lysine in the form of a hydrochloride salt.    -   1.35 Any foregoing composition wherein the composition comprises        0.01%-2.0% lysine hydrochloride.    -   1.36 Any foregoing composition wherein the composition comprises        greater than 50% water.    -   1.37 Any foregoing composition wherein the composition comprises        70% to 95% water.    -   1.38 Any foregoing composition wherein the composition comprises        one or more of a thickener, a buffer, a humectant, a surfactant,        an abrasive, a sweetener, a flavorant, a pigment, a dye, an        anti-caries agent, an anti-bacterial agent, a whitening agent, a        desensitizing agent, a preservative, or a mixture thereof.    -   1.39 Any foregoing composition wherein the composition comprises        a phosphate buffer.    -   1.40 Any foregoing composition wherein the composition comprises        a butler wherein the buffer comprises sodium hydroxide.    -   1.41 Any foregoing composition further comprising a pH        adjustment agent selected from lactic acid, citric acid,        hydrochloric acid, glycolic acid, sodium hydroxide, potassium        chloride, monosodium citrate, disodium citrate, monosodium        malate, sodium carbonate, bicarbonates, sesquicarbonates,        borates, silicates, monosodium phosphate, trisodium phosphate,        pyrophosphate salts, imidazole, or combinations thereof, e.g.,        citric acid.    -   1.42 Any foregoing composition comprising a pH adjustment agent        in an amount of 0.01% to 5.0%, 0.01% to 2.0%, 0.1% to 1.0%, or        about 0.5%.    -   1.43 Any foregoing composition wherein the composition has a pH        of about 1 to 7, about 3 to 6, about 5 to 6, or about 5.25 to        5.75.    -   1.44 Any foregoing composition wherein the composition comprises        a humectant, e.g. selected from sorbitol, propylene glycol,        glycerin, and combinations thereof    -   1.45 Any foregoing composition wherein the composition comprises        a humectant, wherein the humectant is a mixture of glycerin,        sorbitol, and propylene glycol.    -   1.46 Any foregoing composition wherein the composition comprises        an abrasive.    -   1.47 Any foregoing composition wherein the composition comprises        an abrasive, wherein the abrasive comprises silica.    -   1.48 Any foregoing composition wherein the composition a        sweetener.    -   1.49 Any foregoing composition wherein the composition a        sweetener, wherein the sweetener is sodium saccharin.    -   1.50 Any foregoing composition wherein the composition comprises        a flavorant.    -   1.51 Any foregoing composition wherein the composition comprises        a dye, e.g., FD&C Blue No. 1.    -   1.52 Any foregoing composition wherein the composition comprises        an anti-caries agent.    -   1.53 Any foregoing composition wherein the composition comprises        a fluoride ion source.    -   1.54 Any foregoing composition wherein the composition comprises        a fluoride ion source, wherein the fluoride ion source is        stannous fluoride, sodium fluoride, potassium fluoride, sodium        monofluorophosphate, sodium fluorosilicate, ammonium        fluorosilicate, amine fluoride (e.g.,        N′-octadecyltrimethylendiamine-N,N,N′-tris(2-ethanol)-dihydrofluoride),        ammonium fluoride, titanium fluoride, hexafluorosulfate, or a        mixture thereof.    -   1.55 Any foregoing composition wherein the composition comprises        a whitening agent.    -   1.56 Any foregoing composition wherein the composition comprises        a whitening agent, wherein the whitening agent is hydrogen        peroxide.    -   1.57 Any foregoing composition wherein the composition comprises        a desensitizing agent, a vitamin, a preservative, an enzyme, or        a mixture thereof.    -   1.58 Any foregoing composition wherein the composition is a        mouthwash, toothpaste, tooth gel, tooth powder, non-abrasive        gel, mousse, foam, mouth spray, lozenge, oral tablet, dental        implement, or pet care product.    -   1.59 Any foregoing composition wherein the composition is a        mouthwash.    -   1.60 Any foregoing composition which is biphasic, e.g., wherein        the solution comprises two distinct aqueous phases having        different composition and density.    -   1.61 Any foregoing composition which comprises less than 5%,        e.g., less than 2% of hydrophobic ingredients.    -   1.62 Any foregoing composition which is essentially oil-free,        apart from flavoring agents.    -   1.63 Any foregoing composition wherein there is no visible        precipitation or reaction between the short chain polyphosphate        salt and the orally acceptable cationic active agent after three        months of storage at room temperature.    -   1.64 Any foregoing composition for use in any of Methods A-E.    -   1.65 Any foregoing composition obtained or obtainable by Method        F, infra.    -   1.66 Any foregoing composition wherein the composition is a        mouthwash, wherein        -   (i) the short chain polyphosphate salt comprises sodium            tripolyphosphate in an amount of about 0.1 to 5%, e.g.,            0.5-3%, e.g., 1-2%;        -   (ii) the effective amount of orally acceptable cationic            active agent, in free or orally acceptable salt form,            comprises chlorhexidine in an amount of 0.1 to 0.2%;        -   (iii) the anionic surfactant comprises sodium lauryl sulfate            in an amount of 0.1 to 2.0%; and        -   (iv) the amount of water is 70-95%, e.g. 75-85%;        -   wherein the composition further comprises a poloxamer, e.g.,            poloxamer 407, poloxamer 335 or combinations thereof, e.g.            poloxamer 407, in an amount of 0.05-1%, e.g., 0.1-0.3%;        -   wherein the composition further comprises humectant            comprising sorbitol, propylene glycol, glycerin, or            combinations thereof, in an amount of 10-30%, e.g. 15-25%;            and        -   wherein all amounts are by weight of the total composition.

Further claimed is the use of an anionic surfactant, in free or orallyacceptable salt form, to stabilize an oral care formulation comprising ashort chain polyphosphate salt and an effective amount of orallyacceptable cationic active agent, in free or orally acceptable saltform; for example, use in any of the foregoing Compositions 1, et seq.

As used herein, an “oral care composition” refers to a composition forwhich the intended use can include oral care, oral hygiene, or oralappearance, or for which the intended method of use can compriseadministration to the oral cavity. The term “oral care composition” thusspecifically excludes compositions which are highly toxic, unpalatable,or otherwise unsuitable for administration to the oral cavity. In someembodiments, an oral care composition is not intentionally swallowed,but is rather retained in the oral cavity for a time sufficient toaffect the intended utility. The oral care compositions as disclosedherein may be used in nonhuman mammals such as companion animals (e.g.,dogs and cats), as well as by humans. In some embodiments, the oral carecompositions as disclosed herein are used by humans. Oral carecompositions include, for example, dentifrice and mouthwash. In someembodiments, the disclosure provides mouthwash formulations.

As used herein, “orally acceptable” refers to a material that is safeand palatable at the relevant concentrations for use in an oral careformulation, such as a mouthwash or dentifrice.

As used herein, “orally acceptable carrier” refers to any vehicle usefulin formulating the oral care compositions disclosed herein. The orallyacceptable carrier is not harmful to a mammal in amounts disclosedherein when retained in the mouth, without swallowing, for a periodsufficient to permit effective contact with a dental surface as requiredherein. In general, the orally acceptable carrier is not harmful even ifunintentionally swallowed. Suitable orally acceptable carriers include,for example, one or more of the following: water, a thickener, a buffer,a humectant, a surfactant, an abrasive, a sweetener, a flavorant, apigment, a dye, an anti-caries agent, an anti-bacterial, a whiteningagent, a desensitizing agent, a vitamin, a preservative, an enzyme, andmixtures thereof.

As used herein, “short chain polyphosphate salt” encompasses orallyacceptable mono- and polyphosphates, for example, P₁₋₆ phosphates suchas monobasic, dibasic or tribasic orthophosphate; and dimericphosphates, e.g., sodium hexametaphosphate. For example, the short chainpolyphosphate salt may comprise alkali dibasic orthophosphate and alkalipyrophosphate salts, e.g., selected from sodium phosphate dibasic,potassium phosphate dibasic, dicalcium phosphate dihydrate, calciumpyrophosphate, tetrasodium pyrophosphate, tetrapotassium pyrophosphate,sodium tripolyphosphate, and mixtures of any of two or more of these. Ina particular embodiment, for example the compositions comprise a mixtureof tetrasodium pyrophosphate (Na₄P₂O₇), calcium pyrophosphate (Ca₂P₂O₇),and sodium phosphate dibasic (Na₂HPO₄). In one embodiment, tetrasodiumpyrophosphate (TSPP), sodium tripolyphosphate (STPP), tetrapotassiumpyrophosphate (TKPP), or mixtures thereof are used. In anotherembodiment, the compositions comprise a mixture of tetrapotassiumpyrophosphate (TSPP) and sodium tripolyphosphate (STPP)(Na₅P₃O₁₀). Suchphosphates are provided in an amount effective to reduce stains on toothsurfaces, erosion of the enamel, to aid in cleaning the teeth, and/orreduce tartar buildup on the teeth, for example, in an amount of 0.01wt. % to 5.0 wt. %, 0.1 wt. % to 5.0 wt. %, 0.1 wt. % to 3 wt. %, 0.5wt. % to 1.5 wt. %, or 1.0 wt. % based on the total weight of thecomposition.

As used herein, “orally acceptable cationic active agent” means an agentwhich is cationic in aqueous solution at neutral pH and which providessome benefit, e.g. antimicrobial, antigingivitis, and/or antierosionactivity, to the teeth or oral cavity. While in aqueous formulation, theagent will generally be in solution, but it may be introduced to theformulation formulated in free or orally acceptable salt form. Incertain embodiments, the orally acceptable cationic active agent isselected from one or more of quaternary ammonium surfactants (such ascetyl pyridinium chloride (CPC)), bisguanides (such as chlorhexidinedigluconate), cationic amino acids (such as arginine), metal cations(such as zinc, calcium, or stannous ions), or combinations thereof.

As used herein, “anionic surfactant” means those surface-active ordetergent compounds that contain an organic hydrophobic group containinggenerally 8 to 26 carbon atoms or generally 10 to 18 carbon atoms intheir molecular structure and at least one water-solubilizing groupselected from sulfonate, sulfate, and carboxylate so as to form awater-soluble detergent. Usually, the hydrophobic group will comprise aC₈-C₂₂ alkyl, or acyl group. Such surfactants are employed in the formof water-soluble salts and the salt-forming cation usually is selectedfrom sodium, potassium, ammonium, magnesium and mono-, di- or tri-C₂-C₃alkanolammonium, with the sodium, magnesium and ammonium cations againbeing the usual ones chosen. Some examples of suitable anionicsurfactants include, but are not limited to, the sodium, potassium,ammonium, and ethanolammonium salts of linear C₈-C₁₈ alkyl ethersulfates, ether sulfates, and salts thereof. Suitable anionic ethersulfates have the formula R(OC₂H₄)_(n) OSO₃M wherein n is 1 to 12, or 1to 5, and R is an alkyl, alkylaryl, acyl, or alkenyl group having 8 to18 carbon atoms, for example, an alkyl group of C₁₂-C₁₄ or C₁₂-C₁₆, andM is a solubilizing cation selected from sodium, potassium, ammonium,magnesium and mono-, di- and triethanol ammonium ions. Exemplary alkylether sulfates contain 12 to 15 carbon atoms in the alkyl groupsthereof, e.g., sodium laureth (2 EO) sulfate. Some preferred exemplaryanionic surfactants that may be used in the compositions of the presentdisclosure include sodium laurel ether sulfate (SLES), sodium laurylsulfate, and ammonium lauryl sulfate. In certain embodiments, theanionic surfactant is present in an amount of 0.01 to 5.0%, 0.1 to 2.0%,0.2 to 0.4%, or about 0.33%.

As used herein, “nonionic surfactant” generally refers to compoundsproduced by the condensation of alkylene oxide groups (hydrophilic innature) with an organic hydrophobic compound which may be aliphatic oralkyl-aromatic in nature. Examples of suitable nonionic surfactantsinclude poloxamers (sold under trade name PLURONIC®), polyoxyethylene,polyoxyethylene sorbitan esters (sold under trade name TWEENS®),Polyoxyl 40 hydrogenated castor oil, fatty alcohol ethoxylates,polyethylene oxide condensates of alkyl phenols, products derived fromthe condensation of ethylene oxide with the reaction product ofpropylene oxide and ethylene diamine, ethylene oxide condensates ofaliphatic alcohols, alkyl polyglycosides (for example, fatty alcoholethers of polyglycosides, such as fatty alcohol ethers ofpolyglucosides, e.g., decyl, lauryl, capryl, caprylyl, myristyl, stearyland other ethers of glucose and polyglucoside polymers, including mixedethers such as capryl/caprylyl (C₈₋₁₀) glucoside, coco (C₈₋₁₆)glucoside, and lauryl (C₁₂₋₁₆) glucoside), long chain tertiary amineoxides, long chain tertiary phosphine oxides, long chain dialkylsulfoxides, and mixtures of such materials.

In some embodiments, the nonionic surfactant comprises amine oxides,fatty acid amides, ethoxylated fatty alcohols, block copolymers ofpolyethylene glycol and polypropylene glycol, glycerol alkyl esters,polyoxyethytene glycol octylphenol ethers, sorbitan alkyl esters,polyoxyethylene glycol sorbitan alkyl esters, and mixtures thereof.Examples of amine oxides include, but are not limited to,laurylamidopropyl dimethylamine oxide, myristylamidopropyl dimethylamineoxide, and mixtures thereof. Examples of fatty acid amides include, butare not limited to, cocomonoethanolamide, lauramide monoethanolamide,cocodiethanolamide, and mixtures thereof. In certain embodiments, thenonionic surfactant is a combination of an amine oxide and a fatty acidamide. In certain embodiments, the amine oxide is a mixture oflaurylamidopropyl dimethylamine oxide and myristylamidopropyldimethylamine oxide. In certain embodiments, the nonionic surfactant isa combination of lauryl/myristylamidopropyl dimethylamine oxide andcocomonoethanolamide. In certain embodiments, the nonionic surfactant ispresent in an amount of 0.01 to 5.0%, 0.1 to 2.0%, 0.1 to 0.6%, 0.2 to0.4%, about 0.2%, or about 0.5%.

As used herein “polyamine compound” means a molecule having at least twoprimary or secondary amine groups, for example having an isoelectricpoint of greater than pH 8.5, for example pH 9-10. Examples ofpolyamines include ethylene diamine, lysine, or histadine, as well aspolymers such as Lupasol P, which is a polyethylenimine. The polyaminemust be safe for its intended use. Where the composition is an oral carecomposition, the polyamine must be orally acceptable. The polyamine maybe provided in free or acid addition salt form. In certain embodimentsthe polyamine compound is lysine.

As used herein, “biphasic” refers to stable liquid compositions whichcontain at least two distinct homogeneous phases, having differentdensities, such that the phases are separate at rest. The phases may bereadily mixed by shaking but will then re-separate over a short period,e.g., less than half an hour. In certain embodiments, the term excludesgels, emulsions, microemulsions, and homogeneous solutions. In certainembodiments, these formulations differ from conventional biphasicformulations in that both phases are aqueous, rather than one phasebeing hydrophobic and the other hydrophilic.

As used herein, a “tartar control agent” refers to a compound or amixture of compounds that inhibit the formation of tartar, a mixture ofcalcium phosphates on organic matrices, and/or the deposition of plaqueon teeth to form tartar (calculus).

As used herein, “chemical stain” refers to a discoloration of a dentalsurface caused by adsorption or absorption of a colored agent on or intothe surface, or caused by chemical reaction of material of the dentalsurface (e.g., dental enamel) with a colored or noncolored agentcontacting the surface. “Chemical staining” herein means formationand/or development of a chemical stain.

As used herein, “dental surface” refers to a surface of a natural toothor a hard surface of artificial dentition including a crown, cap,filling, bridge, dental implant and the like. In some embodiments, thedental surface is a natural tooth.

The compositions are, for example, oral care compositions, in accordancewith Composition 1, et seq. for example mouthwashes. Any of thecompositions of Composition 1, et seq. is suitable for oral care use,provided the ingredients are orally acceptable. In some embodiments, themouthwash of Composition 1 comprises an effective amount of an orallyacceptable cationic active agent, which is an antimicrobial,antigingivitis, anti-erosion and/or anti-caries agent, e.g. a cationicactive agent selected from one or more of quaternary ammoniumsurfactants (such as cetyl pyridinium chloride (CPC)), bisguanides (suchas chlorhexidine digluconate), cationic amino acids (such as arginine),metal cations (such as zinc, calcium, or stannous ions), or combinationsthereof. The orally acceptable cationic active agent may be present inan effective amount, for example an antimicrobial, antigingivitis,anti-erosion and/or anti-caries amount. The precise amount will dependon the particular active agent and the condition to be treated orprevented, but in various embodiments, antimicrobially effective levelsof CPC in a mouthwash would include amounts from 0.05 to 0.1%, e.g.,about 0.075%; antimicrobially effective levels of chlorhexidinedigluconate in a mouthwash would include amounts from 0.1-0.2%, e.g.,about 0.12%; anti-erosion or anti-microbial levels of metal cations suchas zinc (e.g., zinc citrate or other soluble salt) or stannous (e.g.,stannous fluoride and/or stannous chloride) would be on the order of100-1500 ppm.

The oral care composition used in the present disclosure comprisesignificant levels of water. Water employed in the preparation ofcommercial oral compositions should be deionized and free of organicimpurities. The amount of water in the compositions includes the freewater that is added plus that amount which is introduced with othermaterials.

Mouthwashes frequently contain significant levels of ethanol, which isoften needed to solubilize essential oils and to prevent bacterialcontamination. High levels of ethanol may be undesirable, because inaddition to the potential for abuse by ingestion, the ethanol mayexacerbate conditions like xerostoma. Accordingly, in some embodiments,the oral care compositions of the invention are substantially free ofethanol, e.g., contain less than 1% ethanol.

Humectants can enhance the viscosity, mouthfeel, and sweetness of theproduct, and may also help preserve the product from degradation ormicrobial contamination. Suitable humectants include edible polyhydricalcohols such as glycerin, sorbitol, xylitol, propylene glycol as wellas other polyols and mixtures of these humectants. Sorbitol may in somecases be provided as a hydrogenated starch hydrolysate in syrup form,which comprises primarily sorbitol (the product if the starch werecompletely hydrolyzed to glucose, then hydrogenated), but due toincomplete hydrolysis and/or presence of saccharides other than glucose,may also include other sugar alcohols such mannitol, maltitol, andlonger chain hydrogenated saccharides, and these other sugar alcoholsalso function as humectants in this case. In some embodiments,humectants are present at levels of 5% to 30%, e.g., 10% to 20% byweight.

Flavorings for use in the present invention may include extracts or oilsfrom flavorful plants such as peppermint, spearmint, cinnamon,wintergreen, and combinations thereof, cooling agents such as menthol,methyl salicylate, and commercially available products such as OptaCool®from Symrise, as well as sweeteners, which may include polyols (whichalso function as humectants), saccharin, acesulfame, aspartame, neotame,stevia and sucralose.

Further provided is a method (Method A) for the treatment and/orinhibition of a chemical stain, plaque, and/or tartar on a dentalsurface, comprising contacting the dental surface with any of thepreceding oral care compositions.

Further provided herein is Method A as follows:

-   -   A.1 Method A wherein the composition is Composition 1, e.g.,        selected from any of Compositions 1.1-1.63.    -   A.2 Method A or A.1 wherein the method is for the treatment of a        chemical stain, plaque, and/or tartar on the dental surface.    -   A.3 Method A.2 wherein the method is for the treatment of a        chemical stain on the dental surface.    -   A.4 Method A.2 wherein the method is for the treatment of plaque        on the dental surface.    -   A.5 Method A.2 wherein the method is for the treatment of tartar        on the dental surface.    -   A.6 Method A or A.1 wherein the method is for the inhibition of        a chemical stain, plaque, and/or tartar on the dental surface.    -   A.7 Method A.6 wherein the method is for the inhibition of a        chemical stain on the dental surface.    -   A.8 Method A.6 wherein the method is for the inhibition of        plaque on the dental surface.    -   A.9 Method A.6 wherein the method is for the inhibition of        tartar on the dental surface.    -   A.10 Method A or A.1-A.9 wherein the dental surface is a human        tooth.    -   A.11 Method A or A.1-A.10 wherein the composition is contacted        with the dental surface by brushing.    -   A.12 Any foregoing Method A, et seq. wherein e formulation is bi        phasic and is shaken before use.

Further provided is a method (Method B) for the treatment and/orinhibition of gum disease comprising contacting the oral cavity with anyof the preceding oral care compositions.

Further provided herein is Method B as follows:

-   -   B.1 Method B wherein the composition is Composition 1, e.g., any        of Compositions 1.1-1.63.    -   B.2 Method B or B.1 wherein the method is for the treatment of        gum disease.    -   B.3 Method B, B.1, or B.2 wherein the gum disease is gingivitis.    -   B.4 Method B, B.1, or B wherein the gum disease is        periodontitis.    -   B.5 Method B or B.1 wherein the method is for the inhibition of        gum disease.    -   B.6 Method B, B.1, or B.5 wherein the gum disease is gingivitis.    -   B.7 Method B, B.1, or B.5 wherein the gum disease is        periodontitis.    -   B.8 Method B or B.1-B.7 wherein the oral cavity is a human oral        cavity.    -   B.9 Method B or B.1-B.8 wherein the composition is contacted        with the oral cavity by brushing.    -   B.10 Any foregoing Method B, et seq. wherein the formulation is        biphasic and is shaken before use.

Further provided is a method (Method C) for the treatment and/orinhibition of halitosis comprising contacting the oral cavity with anyof the preceding oral care compositions.

Further provided herein is Method C as follows:

-   -   C.1 Method C wherein the composition is Composition 1, e.g., any        of Compositions 1.1-1.63.    -   C.2 Method C or C.1 wherein the oral cavity is a human oral        cavity.    -   C.3 Method C, C.1, or C.2 wherein the composition is contacted        with the oral cavity by brushing.    -   C.4 Any foregoing Method C, et seq. wherein the formulation is        biphasic and is shaken before use.

Further provided is a method (Method D) for inhibiting biofilm formationon a dental surface comprising contacting the dental surface with any ofthe preceding oral care compositions.

Further provided herein is Method D as follows:

-   -   D.1 Method D wherein the composition is Composition 1, e.g., any        of Compositions 1.1-1.63.    -   D.2 Method D or D.1 wherein the dental surface is a human tooth.    -   D.3 Method D, D.1, or D.2 wherein the composition is contacted        with the dental surface by brushing.    -   D.4 Any foregoing Method D, et seq. wherein the formulation is        biphasic and is shaken before use.

Further provided is a method (Method E) for treating and/or inhibitingbacteria from aggregating and forming bigger colonies in an oral cavitycomprising contacting the oral cavity with any of the preceding oralcare compositions.

Further provided herein is Method E as follows:

-   -   E.1 Method E wherein the composition is Composition 1, e.g., any        of Compositions 1.1-1.63.    -   E.2 Method E or E.1 wherein the oral cavity is a human oral        cavity.    -   E.3 Method E, E.1, or E.2 wherein the composition is contacted        with the oral cavity by brushing.    -   E.4 Any foregoing Method E, et seq. herein the formulation is        biphasic and is shaken before use.

Further provided are Compositions 1, et seq. for use in any of MethodsA-E.

As used herein, “inhibition” refers to reduction of stains that wouldotherwise form or develop subsequent to the time of the treatment. Suchinhibition can range from a small but observable or measurable reductionto complete inhibition of subsequent staining, by comparison with anuntreated or placebo-treated dental surface.

Where the dental surface is substantially free of chemical stains,Method A, e.g., A.1-A.12, is effective to inhibit formation anddevelopment of new chemical stains, as can occur for example by oral useof tobacco products (including smoking) or by drinking tea, coffee, redwine, or cola beverages, subsequent to treatment according to themethod. Where the dental surface already possesses some degree ofchemical staining, Method A, e.g., A.1-A.12, is effective to inhibitfurther development of the existing stain. In some embodiments, theMethod A, e.g., A.1-A.12, can remove, partially or completely, anexisting chemical stain as well as inhibit subsequent staining.

We have further discovered that the formation of precipitating complexesbetween the phosphate and the cationic antibacterial is affected by theorder in which the components are added. If the components are not addedin the correct order, a precipitate is formed that will not redissolve.Thus, in another embodiment, the disclosure provides a method (Method F)of making an oral care composition comprising (i) a short chainpolyphosphate salt [e.g., selected from tripolyphosphates,pyrophosphates and mixtures thereof, e.g. in sodium and/or potassiumsalt form, e.g., selected from sodium tripolyphosphate, potassiumtripolyphosphate, tetrapotassium pyrophosphate, tetrasodiumpyrophosphate, and mixtures of any two or more of these]; (ii) aneffective amount of orally acceptable cationic active agent, in free ororally acceptable salt form [e.g. 0.1-1% of chlorhexidine orchlorhexidine digluconate]; (iii) a stabilizing amount of an anionicsurfactant [e.g., 0.1-1% sodium lauryl sulfate]; (iv) water; andoptionally one or more of a basic amino acid in free or salt form [e.g.0.5-1% lysine or 0.4-0.8% arginine, e.g., as a solid], humectant,nonionic polymer, flavoring and/or dye (e.g., a method of making an oralcare composition according to any of Compositions 1, et seq.); themethod comprising the following steps in the following order:

-   -   a) adding the stabilizing amount of an anionic surfactant to        water;    -   b) adding a dilute solution of the effective amount of orally        acceptable cationic active agent, in free or orally acceptable        salt form, [e.g., adding an aqueous solution having a        concentration of 0.1% to 5%, e.g., 0.5% to 2%, e.g., about 1% of        active] to the product of step a);    -   c) adding the short chain polyphosphate salt in solid form to        the product of step b);    -   d) optionally admixing to the solution thus obtained one or more        of a basic amino acid in free or salt form [e.g. 0.5-1% lysine        or 0.4-0.8% arginine, e.g., as a solid], humectant, nonionic        polymer, flavoring and/or dye;    -   wherein during addition steps a), b) and c), the pH is        maintained between pH 5 and 6, e.g., between pH 5.25-5.75, e.g.        using a pH adjusting agent, e.g. citric acid.

In another embodiment, the disclosure provides an oral care compositionor oral composition premix, comprising (i) a short chain polyphosphatesalt; (ii) an effective amount of orally acceptable cationic activeagent, in free or orally acceptable salt form; (iii) a stabilizingamount of an anionic surfactant; and (iv) water (e.g., an oral carecomposition according to any of Compositions 1, et seq.) obtained orobtainable by the process of Method F.

EXAMPLES Example 1 Chlorhexidine and Anti-stain Polyphosphate Salts

Chlorhexidine (CHX) mouthwash is very effective to fight gingivitis. Butafter CHX has been adsorbed to a tooth surface, stains often resultafter drinking coffee, tea, or red wine, primarily occurring throughcharge interaction between the positively charged CHX and negativelycharged stains. This means that someone using a chlorhexidine musteither avoid foods and beverages with a dark color, or become accustomedto teeth that are more yellow and stained.

Sodium tripolyphosphate (STPP) exhibits significant stain fightingability, and when used in oral care products, deposits onto a toothsurface. However, when STPP and CHX are combined, complexes formed bythe two can result in precipitation of both STPP and CHX, inactivatingboth components.

We have found, however, that CHX and STPP can be formulated in such away to prevent precipitation (or to re-dissolve the precipitate) throughthe inclusion of sodium lauryl sulfate. Additionally, the nonionicsurfactant Poloxamer 407 can be used to supplement portions of SLS. Thefollowing formulations are tested:

TABLE 1 Test formulations Materials Formulation 1 (wt. %) Formulation 2(wt. %) Chlorhexidine 0.6386 (0.1277 active) 0.6386 (0.1277 active)digluconate (20% solution) Poloxamer 407 (nonionic 0.2 0.2 surfactant)Sodium 1.0 1.0 Tripolyphosphate Sodium lauryl sulfate 0.325 0.325(anionic surfactant) Glycerine 7.2 7.2 Sorbitol (70% solution) 9.6 (6.7active) 9.6 (6.7 active) Propylene Glycol 7.0 7.0 Flavor 0.1 0.1 FD&CBlue No. 1 0.0001 0.0001 Citric Acid Monohydrate 0.5 0.5 Lysinehydrochloride — 1.0 Water q.s. q.s.

Method of Preparation: Sodium lauryl sulfate is added as a solid towater, which results in a clear solution as the sodium lauryl sulfatedissolves. A 1% diluted solution of chlorhexidine is then added to thesolution. The chlorhexidine is added dropwise over a period of about oneminute. Sodium tripolyphosphate is then dissolved into the solution. ThepH is maintained between 5.25-5.75 using a pH adjusting agent, such ascitric acid. Poloxamer 407 may then be added to the solution to enhancesolution clarity.

Stain reduction: The efficacy of the test formulations on staining istested against a commercial 0.12% chlorhexidine digluconate (CHX)mouthwash. Table 2 below compares the change in color (ΔW) ofhydroxyapatite (HAP) discs treated with various solutions. Each HAP discis soaked in centrifuged saliva for at least two hours at 37° C. Afterthis time, the discs are rinsed with water and then transferred to thesolutions listed for 15 minutes at 37° C. This is repeated two moretimes for a total of three CHX treatments. The discs are rinsed a finaltime, then put in a coffee/tea/wine solution for 15 minutes with shakingat 37° C. The discs are removed and rinsed, and the change in color (ΔW)is measured.

The results are as follows:

TABLE 2 Stain protection with various formulations 0.12 CHX, 1Compositions Commercial 0.12 CHX, 0.2 STPP, 0.2 P407, (wt. %) 0.12% CHXP407, 0.325 SLS 0.325 SLS ΔW 35.3 24.5 14.9 CHX = chlorhexidinedigluconate; SLS = sodium lauryl sulfate (anionic surfactant); P407 =poloxamer 407 (nonionic surfactant); STPP = sodium tripolyphosphate.As expected, the discs treated with commercial chlorhexidine mouthwashand red wine exhibit considerable staining. Combining CHX with thesurfactant combination SLS and P407 consistently provides a degree ofstain prevention. However, when STPP is included in the formulation, ΔWdecreases by about 50%, which is a significant increase in stainpreventing power.

Bacterial kill: A 20-second short interval kill test (SIKT) measures theefficacy of various treatment solutions in killing oral pathogens. TheFluorescent SIKT uses Live/Dead BacLight fluorescent viability stainingsystem to measure permeabilization of bacteria by single actives orliquid formulations. A mixed species inoculum culture containing:Lactobacillus casei, Streptococcus oralis, Actinomyces viscosus,Veillonella parvula & Fusobacterium nucleatum at an optical density of0.5@610 nm is centrifuged. The supernatant is then aspirated off and theremaining pellicle is re-suspended in sterile phosphate buffered saline(PBS). 100 μl of this solution is then treated with 100 μl of testsample for 30 or 60 seconds. Immediately following treatment, theexposure is neutralized by adding 1.3 ml of sterile D/E neutralizingbroth. The neutralizing broth is then rinsed off by centrifugation andre-suspension in PBS. 50 μl samples are then transferred in triplicateto a 96-well microplate. The fluorescent dyes are then prepared per themanufacturer's directions and added to the samples. The fluorescence isthen measured in a fluorescent plate reader. Data from this assay arepresented as a percentage of bacterial remaining viable relative to acontrol sample treated with PBS. The formulations containing Poloxamer407 and STPP provided a reduction of about 70% reduction in bacterialviability vs. about 50% for a commercial formulation lacking theseingredients. The percent viability of different formulations, whereinlower percent viability corresponds higher bacteriocidal activity, isset forth in table 3.

TABLE 3 SIKT with different formulations 1.0 STPP, 0.2 1.0 STPP, 0.5Compositions Commercial P407, 0.325 P407, 0.325 (wt. %) 0.12% CHX SLS,0.12 CHX SLS, 0.12 CHX % viability 50.5 29.6 32.9

Example 2

Stain Deposition: Saliva-coated hydroxyapatite (HAP) disks are treatedwith either the commercial CHX mouthwash formulation or Formulation 1,as used in Example 1, and the disks are then challenged with a stainingsolution containing a coffee, tea and wine mixture. Briefly, HAP disksare incubated in 1 mL of saliva in a shaker bath, 37° C., overnight.After rinsing with distilled water, baseline spectrophotometermeasurements are taken. 2 mL of the test formulation is added and thedisk is incubated in the shaker bath at 37° C. for 30 seconds. Afterrinsing with distilled water, spectrophotometer measurements arerepeated. 2 mL of the stain solution is then added, and the disks areincubated in the shaker bath at 37° C. for 15 min. After rinsing withdistilled water, spectrophotometer measurements are taken again. Thistreatment/stain procedure is repeated for a total of three stainingcycles. The spectrophotometer measurements are used to evaluate changein color values (abL). Stain prevention efficacy is measured asΔE(Et−Ei) and/or ΔW*(W*t−W*i) according to known methods. The resultsare shown in Table 4 below. The results demonstrate that Formulation 1is significantly more effective in preventing stain deposition than thecommercial CHX formulation.

TABLE 4 Commercial Formulation 1 Stain Cycle CHX (ΔW) (ΔW) First 17.47.7 Second 24.6 15.2 Third 29.5 21.0

Bacterial Kill Efficacy: A five-day biofilm assay is performed tocompare the efficacy of Formulation 1 with and without chlorhexidine inthe presence of sodium lauryl sulfate. The active attachment biofilmmodel (Extrecate et al., Caries Research 2010; 44:372-379) is used tomeasure the antibacterial efficacy of the mouthwash formulations. Inthis model, 24 hydroxyapatite (HAP) discs are clamped onto a sterilemetal lid. The lid is then inoculated in 2% unstimulated saliva inMcBain medium for 24 hours at 37° C. on a 24-well plate under anaerobicconditions. After initial attachment, the biofilms are transferred intofresh growth media for maturation. Treatment is performed afterformation of a 24 hour biofilm. The HAP discs are treated for 10 minutesat room temperature in 1.6 ml of the mouthwash formulation. The lid issubsequently transferred to a new plate for washing with 1.7 ml 25%Tryptic Soy Buffer and moved up and down 10 times. The wash step isrepeated three times. The biofilms are then transferred into McBainmedium and incubated anaerobically at 37° C. The discs are treated seventimes over a 5-day period and the resulting biofilms are harvested usingsonication. The harvested biofilms are subjected to ATP metabolic assay(Life Technology) and plated on 5% sheep blood agar plate to determinetotal colony counts. The results are reported as log(CFU/ml) for fourreplicates of each sample. The results are shown in Table 5 below. Theseresults demonstrate that the chlorhexidine present in Formulation 1 iseffective at killing bacteria despite the presence of sodium laurylsulfate.

TABLE 5 Formula Log CFU/mL Untreated 9.59 control Formulation 1 8.02without CHX Formulation 1 6.06

The invention claimed is:
 1. An oral care composition comprising a) ashort chain polyphosphate salt, wherein the short chain polyphosphatesalt comprises sodium tripolyphosphate or tetrapotassium pyrophosphate;b) an effective amount of orally acceptable cationic active agent, infree or orally acceptable salt form, wherein the orally acceptablecationic active agent comprises chlorhexidine digluconate; c) astabilizing amount of an anionic surfactant, wherein the anionicsurfactant comprises sodium laureth sulfate, sodium lauryl sulfate,ammonium lauryl sulfate, or combinations thereof; and d) water.
 2. Thecomposition of claim 1 wherein the short chain polyphosphate saltcomprises sodium tripolyphosphate, at a concentration of 0.1 wt. %-5.0wt. %.
 3. The composition of claim 1 wherein the orally acceptablecationic active agent further comprises one or more of quaternaryammonium surfactants, bisguanides, cationic amino acids, metal cations,guanidinium polymers, and combinations thereof.
 4. The composition ofclaim 1 wherein the orally acceptable cationic active agent furthercomprises an orally acceptable salt selected from zinc salts, stannoussalts, and cetyl pyridinium chloride.
 5. The composition of claim 1wherein chlorhexidine digluconate is present, at a concentration of 0.1wt. %-0.2 wt. %.
 6. The composition of claim 1 wherein the anionicsurfactant comprises sodium lauryl sulfate, at a concentration of 0.1wt. %-1.0 wt. %.
 7. The composition of claim 1 further comprising anonionic surfactant.
 8. The composition of claim 1 wherein thecomposition comprises 70% to 95% water.
 9. The composition of claim 1wherein the composition comprises one or more of a thickener, a buffer,a humectant, a surfactant, an abrasive, a sweetener, a flavorant, apigment, a dye, an anti-caries agent, an anti-bacterial agent, awhitening agent, a desensitizing agent, a preservative, or a mixturethereof.
 10. The composition of claim 1 wherein the composition is amouthwash.
 11. The composition of claim 10 which is biphasic, whereinthe solution comprises two distinct aqueous phases having differentcomposition and density.
 12. The composition of claim 1 wherein there isno visible precipitation or reaction between the short chainpolyphosphate salt and the orally acceptable cationic active agent afterthree months of storage at room temperature.
 13. A method for a) thetreatment and/or inhibition of a chemical stain, plaque, and/or tartaron a dental surface, b) the treatment and/or inhibition of gum disease,c) the treatment and/or inhibition of halitosis, d) inhibiting biofilmformation on a dental surface, and/or e) treating and/or inhibitingbacteria from aggregating and forming bigger colonies in an oral cavitycomprising contacting a dental surface with a composition accordingclaim
 1. 14. A method of making an oral care composition according toclaim 1, and optionally, further optionally comprising one or more of abasic amino acid in free or salt form, humectant, nonionic polymer,flavoring and/or dye, wherein the method comprises the following stepsin the following order: a) adding the stabilizing amount of an anionicsurfactant to the water; b) adding a dilute solution of the effectiveamount of orally acceptable cationic active agent, in free or orallyacceptable salt form, to the product of step a); c) adding the shortchain polyphosphate salt in solid form to the product of step b); d)optionally admixing to the solution thus obtained, one or more of abasic amino acid in free or salt form, humectant, nonionic polymer,flavoring and/or dye; wherein during addition steps a), b) and c), thepH is maintained between pH 5 and pH
 6. 15. An oral care compositionwhich is obtained or obtainable by the method of claim
 14. 16. Thecomposition of claim 1, wherein the short chain polyphosphate saltcomprises sodium tripolyphosphate at a concentration of 0.1 wt. %-5.0wt. %, chlorhexidine digluconate is at a concentration of 0.1 wt. %-0.2wt. %, and the anionic surfactant comprises sodium lauryl sulfate at aconcentration of 0.1 wt. %-1.0 wt. %.